- Computer-Aided Fragment Growing Strategies to Design Dual Inhibitors of Soluble Epoxide Hydrolase and LTA4 Hydrolase
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Multitarget ligands are interesting candidates for drug discovery and development due to improved safety and efficacy. However, rational design and optimization of multitarget ligands is tedious because affinity optimization for two or more targets has to be performed simultaneously. In this study, we demonstrate that, given a molecular fragment, which binds to two targets of interest, computer-aided fragment growing can be applied to optimize compound potency, relying on either ligand- or structure-derived information. This methodology is applied to the design of dual inhibitors of soluble epoxide hydrolase and leukotriene A4 hydrolase.
- Hefke, Lena,Hiesinger, Kerstin,Kramer, Jan S.,Proschak, Ewgenij,Zhu, W. Felix
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p. 1244 - 1249
(2020/07/04)
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- The total syntheses of JBIR-94 and two synthetic analogs and their cytotoxicities against A549 (CCL-185) human small lung cancer cells
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We here disclose the total syntheses of the natural polyphenol JBIR-94 and two nonnatural analogs, whose structures are of interest for their bioactivity potential as radical scavengers. Although we initially attempted this by dually acylating both of putrecine's amine nitrogens in a single pot, our endeavors with this method (which has been successfully reported by other groups) proved ineffectual. We accordingly opted for the lengthier approach of acylating each amine individually, which gratuitously prevailed and also aligns with separate literature precedent. Moreover, we here share our analysis of these target compounds’ cytotoxicities and IC50 values against A549 (CCL-185) human small lung cancer cells.
- Mangum, Cathy L.,Munford, Mica B.,Sam, Alyssa B.,Young, Sandra K.,Beales, Jeremy T.,Subedi, Yagya Prasad,Mangum, Chad D.,Allen, Tanner J.,Liddell, Miranda S.,Merrell, Andrew I.,Saavedra, Diana I.,Williams, Becky L.,Evans, Nicole,Beales, Joseph L.,Christiansen, Michael A.
-
supporting information
(2019/11/29)
-
- Benzoic hydroxamate-based iron complexes as model compounds for humic substances: Synthesis, characterization and algal growth experiments
-
A series of monomeric and dimeric FeIII complexes bearing benzoic hydroxamates as O,O-chelates has been prepared and characterized by elemental analysis, IR spectroscopy, UV-Vis spectroscopy, electrospray ionization mass spectrometry (ESI-MS), cyclic voltammetry, EPR spectroscopy and for some examples by X-ray diffraction analysis. The stability of the synthesized complexes in pure water and seawater was monitored over 24 h by means of UV-Vis spectrometry. The ability to release iron from the synthesized model complexes has been investigated with algae growth experiments.
- Orlowska, Ewelina,Roller, Alexander,Wiesinger, Hubert,Pignitter, Marc,Jirsa, Franz,Krachler, Regina,Kandioller, Wolfgang,Keppler, Bernhard K.
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p. 40238 - 40249
(2016/05/24)
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- COMPOUND EXHIBITING REGULATORY ACTIVITY ON LYSOPHOSPHATIDYLSERINE RECEPTOR FUNCTION
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The object of the present invention is to provide a compound having a lysophosphatidylserine receptor function modulation activity or a salt thereof. A compound having a lysophosphatidylserine receptor function modulation activity or a salt thereof, or a pharmaceutical composition or a lysophosphatidylserine receptor function moderator containing such compound or salt is provided by the present invention.
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- POLYMERIZABLE CHIRAL COMPOUND
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The present invention refers to, a strong HTP and a, a lower melting point as chiral compounds having a diffusion barrier it is an object to provide an 1/10 time as large as that of. Said liquid crystal aberration correcting element, general formula (I) Polymerizable chiral reagent represented by compound. Subject to the compounds of the invention herein having a melting and low HTP, since a color compound melting portion of the electron emitting material paste excellent drives liquid crystal composition, is useful as a components. Furthermore, as a component compound polymerizable chiral reagent of the invention herein a polymerizable liquid crystal composition, to produce large-sized content of compound polymerizable chiral reagent of the insertion part and the holder and having excellent optical characteristics and operating method of anisotropic body group represented by the formula 1.. A optically anisotropic product, of the invention herein, the deflecting plates, retardation plate and the like useful.
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-
Paragraph 0185; 0186
(2016/10/10)
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- Synthesis of the alkaloid tyroscherin by an aldol/Curtius strategy
-
The alkaloid tyroscherin (2), which contains a vicinal anti-amino alcohol subunit was prepared from 4-hydroxyphenylpropionic acid (5) and meso-diol 9. After desymmetrization of diol 9 and suitable protecting group manipulations, one terminus was extended via a Claisen rearrangement giving rise to enoate ent-15. The missing carbon on the other end could be incorporated using MeMgCl/CuBr·SMe2 leading eventually to aldehyde ent-22. The acylated oxazolidinone 32 derived from acid 5 and aldehyde ent-22 were combined in an aldol reaction. A subsequent Curtius rearrangement on the carboxylic group furnished the amino function of tyroscherin (2). In a proof of concept study the same strategy was used to prepare tyroscherin analog 28.
- Ugele, Markus,Maier, Martin E.
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supporting information; experimental part
p. 2633 - 2641
(2010/05/01)
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- Structure-activity study of dihydrocinnamic acids and discovery of the potent FFA1 (GPR40) agonist TUG-469
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The free fatty acid 1 receptor (FFA1 or GPR40), which is highly expressed on pancreatic β-cells and amplifies glucose-stimulated insulin secretion, has emerged as an attractive target for the treatment of type 2 diabetes. Several FFA1 agonists containing the para-substituted dihydrocinnamic acid moiety are known. We here present a structure-activity relationship study of this compound family suggesting that the central methyleneoxy linker is preferable for the smaller compounds, whereas the central methyleneamine linker gives higher potency to the larger compounds. The study resulted in the discovery of the potent and selective full FFA1 agonist TUG-469 (29).
- Christiansen, Elisabeth,Due-Hansen, Maria E.,Urban, Christian,Merten, Nicole,Pfleiderer, Michael,Karlsen, Kasper K.,Rasmussen, Sanne S.,Steensgaard, Mette,Hamacher, Alexandra,Schmidt, Johannes,Drewke, Christel,Petersen, Rasmus Koefoed,Kristiansen, Karsten,Ullrich, Susanne,Kostenis, Evi,Kassack, Matthias U.,Ulven, Trond
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scheme or table
p. 345 - 349
(2010/12/19)
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- NOVEL POLYSPIRANE COMPOUNDS, APPLICATION THEREOF IN THE TREATMENT OF MALARIA OR TOXOPLASMOSIS AND METHOD FOR PREPARING SAME
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Novel polyspirane compounds used in the treatment of diseases involving parasites that belong to the phylum of apicomplexae, and a method for preparing the same.
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Page/Page column 17
(2010/12/29)
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- Synthesis of the pyoverdin chromophore by a biomimetic oxidative cyclization
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The fluorescent dihydropyrimido[1,2-a]quinoline chromophore of the pyoverdin siderophores has been synthesized by a biomimetic oxidative cyclization using an iodine (III) reagent, followed by elimination and dehydrogenation.
- Jones, Raymond C.F.,Yau, Sze Chak,Iley, James N.,Smith, Janet E.,Dickson, James,Elsegood, Mark R.J.,McKee, Vickie,Coles, Simon J.
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scheme or table
p. 1519 - 1522
(2009/09/06)
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- TETRACYCLIC INHIBITORS OF FATTY ACID AMIDE HYDROLASE
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Certain tetracyclic compounds are described, which may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).
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- Discovery of azetidinone acids as conformationally-constrained dual PPARα/γ agonists
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A novel class of azetidinone acid-derived dual PPARα/γ agonists has been synthesized for the treatment of diabetes and dyslipidemia. The preferred stereochemistry in this series for binding and functional agonist activity against both PPARα and PPARγ receptors was shown to be 3S,4S. Synthesis, in vitro and in vivo activities of compounds in this series are described. A high-yielding method for N-arylation of azetidinone esters is also described.
- Wang, Wei,Devasthale, Pratik,Farrelly, Dennis,Gu, Liqun,Harrity, Thomas,Cap, Michael,Chu, Cuixia,Kunselman, Lori,Morgan, Nathan,Ponticiello, Randy,Zebo, Rachel,Zhang, Litao,Locke, Kenneth,Lippy, Jonathan,O'Malley, Kevin,Hosagrahara, Vinayak,Zhang, Lisa,Kadiyala, Pathanjali,Chang, Chiehying,Muckelbauer, Jodi,Doweyko, Arthur M.,Zahler, Robert,Ryono, Denis,Hariharan, Narayanan,Cheng, Peter T.W.
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p. 1939 - 1944
(2008/09/20)
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- Enhanced antimalarial activity of novel synthetic aculeatin derivatives
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We report the design, synthesis, and in vitro evaluation of novel polyspirocyclic structures, inspired by the antimalarial natural products, the aculeatins. A divergent synthetic strategy was conceived for the practical supply and has allowed the discover
- Peuchmaur, Marine,Sa?dani, Nadia,Botté, Cyrille,Maréchal, Eric,Vial, Henri,Wong, Yung-Sing
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supporting information; experimental part
p. 4870 - 4873
(2009/07/25)
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- Structure-activity relationships of α-ketooxazole inhibitors of fatty acid amide hydrolase
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A systematic study of the structure-activity relationships of 2b (OL-135), a potent inhibitor of fatty acid amide hydrolase (FAAH), is detailed targeting the C2 acyl side chain. A series of aryl replacements or substituents for the terminal phenyl group provided effective inhibitors (e.g., 5c, aryl = 1-napthyl, K, - 2.6 nM), with 5hh (aryl -3-ClPh, Ki = 900 pM) being 5-fold more potent than 2b. Conformationally restricted C2 side chains were examined, and many provided exceptionally potent inhibitors, of which 11j (ethylbiphenyl side chain) was established to be a 750 pM inhibitor. A systematic series of heteroatoms (O, NMe, S), electron-withdrawing groups (SO, SO2), and amides positioned within and hydroxyl substitutions on the linking side chain were investigated, which typically led to a loss in potency. The most tolerant positions provided effective inhibitors (12p, 6-position S, Ki = 3 nM, or 13d, 2-position OH, Ki = 8 nM) comparable in potency to 2b. Proteome-wide screening of selected inhibitors from the systematic series of >100 candidates prepared revealed that they are selective for FAAH over all other mammalian serine proteases.
- Hardouin, Christophe,Kelso, Michael J.,Romero, F. Anthony,Rayl, Thomas J.,Leung, Donmienne,Hwang, Inkyu,Cravatt, Benjamin F.,Boger, Dale L.
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p. 3359 - 3368
(2008/02/13)
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- Synthesis of two dipeptide isosteres containing di- and trisubstituted E-configured double bonds
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The stereoselective syntheses of a Tyr-Tyr and a Pro-Pro E-alkene isostere are described. While the Tyr-Tyr isostere was synthesized following a convergent olefination strategy, the trisubstituted E-configured double bond of the Pro-Pro isostere was generated by an Ireland-Claisen rearrangement. The configuration of all key intermediates containing new stereocenters was determined by X-ray crystallography. Georg Thieme Verlag Stuttgart.
- Bandur, Nina G.,Harms, Klaus,Koert, Ulrich
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p. 2720 - 2730
(2008/03/12)
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- First stereoselective synthesis of a Tyr-Tyr E-alkene isostere
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A stereoselective synthesis of a tyrosine-tyrosine E-alkene isostere is described. Starting from N-Fmoc-O-(tert-butyl)tyrosine as N-terminal component, the E double bond was generated by a Julia-Kocieński olefination. An enantioselective aldol reaction wa
- Bandur, Nina G.,Harms, Klaus,Koert, Ulrich
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- AGENT FOR CONTROLLING FUNCTION OF GPR34 RECEPTOR
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The present invention provides a GPR receptor function regulator comprising the compound represented by the formula: [wherein ring A is an optionally substituted isocyclic or heterocyclic ring, P is a bond or spacer, ring D is an optionally substituted monocyclic aromatic ring which may be condensed with a 5-to 7-membered ring, V is a bond or the group represented by the formula -CR14=CR15 - or - N=CR16- (wherein R14, R15 and R16 each represents a hydrogen atom or optionally substituted hydrocarbon group), Q is a bond or spacer, and W is a carboxyl or a group biologically equivalent to a carboxyl] or its salt or a prodrug thereof
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Page/Page column 81
(2010/11/28)
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- Melanocortin receptor ligands
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Disclosed are MC-4 and/or MC-3 receptor ligands, the ligands having a structure according to Formula (I): wherein R2, R4, R4′, R5, R6, R6′, R7, R8, R8′, R9, R9′, R10, Ar, Z1, Z2, Z3, X, B, D, p, q, r and s are as described in the specification and claims, and optical isomers, diastereomers or enantiomers thereof; pharmaceutically-acceptable salts, hydrates, and biohydrolyzable esters, amides or imides thereof. Also disclosed are pharmaceutical compositions comprising the ligands of Formula (I), as well as methods of treating diseases mediate by the MC-4/MC-3 receptors, as described in the Detailed Descriptions section of the specification.
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Page/Page column 59
(2010/11/08)
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- Galanthamine analogs: 6H-benzofuro[3a,3,2,-e,f][1]benzazepine and 6H-benzofuro[3a,3,2-e,f][3]benzazepine
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The known cholinesterase inhibitory capability of the Amarylidaceae alkaloid galanthamine prompted preparation of analogs in which the position of the nitrogen within the azepine ring is altered. The analogs 6H-benzofuro[3a,3,2-e,f][1]benzazepine and 6H-benzofuro[3a,3,2-e,f][3] benzazepine were prepared in 19 and 2.5%, respectively, following Kametani and Shimizu approaches, respectively. The aniline derivative 6H-benzofuro[3a,3,2-e, f][1]benzazepine failed to undergo most of the reactions typical for galanthamine. Thus, it neither oxidized to the analogous narwedine, nor epimerized to the analogous epigalanthamine, nor reduced to the lycoramine analog, under the conditions used for galanthamine.
- Lewin, Anita H.,Szewczyk, Jerzy,Wilson, Joseph W.,Carroll, F. Ivy
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p. 7144 - 7152
(2007/10/03)
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- RECEPTOR FUNCTION CONTROLLING AGENT
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The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.
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- Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same
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The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1 and R2, are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula 1, and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
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Page/Page column 153
(2008/06/13)
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- INHIBITORS OF HEPATITIS C VIRUS RNA-DEPENDENT RNA POLYMERASE, AND COMPOSITIONS AND TREATMENTS USING THE SAME
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The invention relates to compounds of the formula (I) and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R1and R2, are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula (I), and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula (I). The invention also relates to methods of preparing the compounds of formula (I).
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- INHIBITORS OF HEPATITIS C VIRUS RNA-DEPENDENT RNA POLYMERASE, AND COMPOSITIONS AND TREATMENTS USING THE SAME
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Compounds of formula (I) are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virus.
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Page/Page column 16
(2010/02/07)
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- Alpha-and beta- substituted trifluoromethyl ketones as phospholipase inhibitors
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Inhibitors of the cytosolic phospholipase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula where X, Z, R1, R2, R3, R4, Ra and Rb are as defined in the specification.
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- Alpha-and beta-substituted trifluoromethyl ketones as phospholipase inhibitors
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Inhibitors of the cytosolic phospholipase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula where X, Z, R1, R2, R3, R4, Raand Rbare as defined in the specification.
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- Discovery of macrocyclic hydroxamic acids containing biphenylmethyl derivatives at P1′, a series of selective TNF-α converting enzyme inhibitors with potent cellular activity in the inhibition of TNF-α release
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SAR exploration at P1′ using an anti-succinate-based macrocyclic hydroxamic acid as a template led to the identification of several bulky biphenylmethyl P1′ derivatives which confer potent porcine TACE and anti-TNF-α cellular activities with high selectivity versus most of the MMPs screened. Our studies demonstrate for the first time that TACE has a larger S1′ pocket in comparison to MMPs and that potent and selective TACE inhibitors can be achieved by incorporation of sterically bulky P1′ residues.
- Xue,He,Corbett,Roderick,Wasserman,Liu,Jaffee,Covington,Qian,Trzaskos,Newton,Magolda,Wexler,Decicco
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p. 3351 - 3354
(2007/10/03)
-
- Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles
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A nonpeptidyl GnRH receptor antagonist (1), with a unique 2-arylindole core, was identified through the Merck in-house screening for binding affinity on the rat GnRH receptor. SAR studies directed toward the alkoxy-ethanolamine and 2-aryl groups resulted in a simpler lead structure with improved activity. This compound 50 exhibits a 60-fold improvement in binding activity over our initial lead 1.
- Chu, Lin,Hutchins, Jennifer E.,Weber, Ann E.,Lo, Jane-Ling,Yang, Yi-Tien,Cheng, Kang,Smith, Roy G.,Fisher, Michael H.,Wyvratt, Matthew J.,Goulet, Mark T.
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p. 509 - 513
(2007/10/03)
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- Nonpeptidic HIV protease inhibitors possessing excellent antiviral activities and therapeutic indices. PD 178390: A lead HIV protease inhibitor
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With the insight generated by the availability of X-ray crystal structures of various 5,6-dihydropyran-2-ones bound to HIV PR, inhibitors possessing various alkyl groups at the 6-position of 5,6-dihydropyran-2-one ring were synthesized. The inhibitors pos
- Vara Prasad,Boyer, Frederick E.,Domagala, John M.,Ellsworth, Edmund L.,Gajda, Christopher,Hamilton, Harriet W.,Hagen, Susan E.,Markoski, Larry J.,Steinbaugh, Bruce A.,Tait, Bradley D.,Humblet, Christine,Lunney, Elizabeth A.,Pavlovsky, Alexander,Rubin, John R.,Ferguson, Donna,Graham, Neil,Holler, Tod,Hupe, Donald,Nouhan, Carolyn,Tummino, Peter J.,Urumov,Zeikus, Eric,Zeikus, Greg,Gracheck, Stephen J.,Saunders, James M.,Vanderroest, Steven,Brodfuehrer, Joanne,Iyer,Sinz,Gulnik, Sergei V.,Erickson, John W.
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p. 2775 - 2800
(2007/10/03)
-
- Kinetics and Mechanism of the Alkaline Hydrolysis of Pentachlorophenyl ω-(p-Hydroxyphenyl)alkanoates
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A kinetic study of the alkaline hydrolysis of pentachlorophenyl esters of ω-(p-hydroxyphenyl)alkanoic acids 3 shows that the dissociative route involving a spirodienone intermediate is not a feasible alternative to the normal associative BAC2 pathway.
- Cevasco, Giorgio,Thea, Sergio
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p. 269 - 272
(2007/10/03)
-
- Head-to-Tail Connected Double Calix[4]arenes
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New macrotricyclic compounds consisting of two calix[4]arene substructures connected by aliphatic chains of various length (three to five carbon atoms) between two opposite p-positions and two distal phenolic oxygens have been synthesized. Starting with p-tert-butyl-calix[4]arene, two O-protected phenolic units are attached via ether links in 1,3-position by reaction with the corresponding tosylates. After deprotection, the new calix[4]arene is formed by fragment condensation with 2,6-tobromomethylated 4-alkylphenols. The structure of one example (8c) has been confirmed by single crystal X-ray analysis. Both calixarene parts assume the cone conformation, a molecule of acetonitrile being included in both cavities.
- Wasikiewicz,Rokicki,Kielkiewicz,Paulus,Boehmer
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p. 863 - 879
(2007/10/03)
-
- Polymer-Supported Mitsunobu Ether Formation and its Use in Combinatorial Chemistry
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Aromatic hydroxy acids have been attached to a polymeric solid support and the phenolic hydroxy groups have been reacted with a variety of primary and secondary alcohols under the conditions of the Mitsunobu reaction (triphenylphosphine and diethyl azodicarboxylate) in tetrahydrofuran.In most cases the reaction provided a nearly quantitative yield of alkyl aryl ethers, as determined after cleaving theproduct from the resin.To demonstrate that the polymer-supported Mitsunobu reaction is useful for combinatorial library synthesis, we synthesized a number of model compounds and a simple three randomization step library composed of 4,200 different compounds.
- Krchnak, Viktor,Flegelova, Zuzka,Weichsel, Aleksandra S.,Lebl, Michal
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p. 6193 - 6196
(2007/10/02)
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- The Effect of Carbonyl Containing Terminal Chains on Mesomorphic Properties in 4,4'-Disubstituted Phenylbenzoates and Phenylthiobenzoates. 4. Phenylbenzoates Containing A (CH2)nCO2R' Group (n = 0-2) on the Phenolic End
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The effect of a (CH2)nCO2R' group on the mesomorphic properties of the esters where X = alkyl or alkoxy, Y = (CH2)nCO2R'(R' = C7 and C9) and n = 0-2 has been studied by synthesizing these esters and determining their mesomorphic properties by hot-stage polarizing microscopy.The starting phenols were prepared by esterification of 4-hydroxybenzoic, phenylacetic or phenylpropionic acids.Both the benzyl and methoxycarbonyl protecting groups were tried with the latter giving higher yields when n = 0 because of better solubility of the protected acid.No mesophases were observed in the esters when n = 1, nematic and smectic A phases occurred when n = 2 and smectic A and C phases when n = 0.A few 1,4-cyclohexane diesters were also prepared using these phenols.The mesomorphic properties of these esters followed the same trend observed in the phenylbenzoates escept no C phases were observed.Comparisons of the transition temperatures for these esters with those for Y = R' showed that both small increases or decreases were observed for Y = CO2R'.However, the addition of a spacer methylene group (n = 1 and 2) always gave lower temperatures with the amount of lowering being much greater for n = 2 than n = 1.A comparison of transition temperatures for Y = CO2R', OCOR', COR' and OR' indicated that these temperatures were higher when Y = COR' as expected from dipole moment considerations but were lower when Y = CO2R' than when Y = OCOR', the opposite expected from these considerations.This trend was also observed in the cyclohexane diesters.Transition temperatures were always higher for the esters when Y has an oxygen atom adjacent to the benzene ring.Therefore, esters with Y = O(CH2)nCO2R', n = 1 and 2 were also synthesized.The phenols were prepared by alkylation of 4-benzyloxyphenol with the bromo esters followed by hydrogenolysis.However, these esters showed no mesophases except the cyclohexane diester with n = 2.
- Neubert, M. E.,Leung, K.,Jirousek, M. R.,Ezenylimba, M. C.,Sabol-Keast, S.,et al.
-
-
- Peptide derivatives
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New peptide derivatives represented by the following general formula wherein R1 is a hydrophobic radical, R2 is a hydrophilic radical, Pro is prolyl and Hyp is hydroxyprolyl show more powerful inhibitory action against platelet a
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- Studies on the Chemical Constituents of Rutaceous Plants. Part 45. Novel Phenyl Propanoids: Cuspidiol, Boninenal, and Methyl Boninenalate
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Cuspidiol, boninenal, and methyl boninenalate were established as having the structures 3-phenyl>propanol (1), (E)-3-phenyl>propenal (2), and (E)-3-phenyl>propenal (3) respectively.The three compounds were also independently synthesized.
- Ishii, Hisashi,Ishikawa, Tsutomu,Tohojoh, Toshiaki,Murakami, Keiko,Kawanable, Eri,et al.
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p. 2051 - 2058
(2007/10/02)
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- THE SYNTHESIS OF ARYLPROPIONIC ACIDS AND THE QUANTITATIVE RELATIONSHIP BETWEEN THE STRUCTURE AND THE ACTIVATION OF FIBRINOLYSIS
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A number of substituted 2-arylpropionic (IV) and 3-arylpropionic (V) acids were prepared and their activity in the activation of fibrinolysis and the inhibition of heat denaturation of serum albumin was evaluated.The results were worked up using the method of regression analysis.From the regression equation obtained it may be considered that both activities are affected mainly by the lipophilicity of the aromatic substituents.The effect of branching in the connecting chain between the carboxyl group and the aromatic ring is negligible in both activities.Thelinear dependence of the fibrinolytic capacity on lipophilicity is in both series of acids, IV and V, characterized by a distinct decrease in activity, following the attainment of the optimum value of lipophilicity.In the series of cinnamic acids (VI) regression equations concerning the inhibition of the denaturation of serum albumin and the activation of fibrinolysis were also calculated, showing a linear dependence of these activities on the lipophilicity of the varying substituents R and X.Summary regression equations were derived for both activities in the whole set of acids I-VI.Both the inhibition of the denaturation of serum albumin , and the activation of fibrinolysis depends on the lipophilicity of the mentioned acids exclusively.The modification of the connecting chain between the carboxyl group and the aromatic ring affects both activities primarily by the corresponding change in lipophilicity.
- Kuchar, Miroslav,Brunova, Bohumila,Rejholec, Vaclav,Roubal, Zdenek,Nemecek, Oldrich
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p. 1173 - 1187
(2007/10/02)
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